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Assay Detail

CHEMBL646605

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding affinity at human Adenosine A3 receptor expressed in HEK 293 cells by [125I]AB-MECA displacement.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Adenosine receptor A3 (CHEMBL256)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

N6,5'-Disubstituted adenosine derivatives as partial agonists for the human adenosine A3 receptor.
van Tilburg EW, von Frijtag Drabbe Künzel J, de Groote M, Vollinga RC, Lorenzen A, IJzerman AP.
J Med Chem (1999) 42 : 1393 -1400
PubMed 10212125 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.00 8.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL606312 1 8.11
CHEMBL2113427 1 8.06
CHEMBL2113428 1 7.76
CHEMBL66393 1 7.56
CHEMBL604636 1 7.51
CHEMBL605468 1 7.39
CHEMBL2113432 1 7.35
CHEMBL2113441 1 7.33
CHEMBL2113468 1 7.13
CHEMBL263643 1 7.05
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 6.92
CHEMBL2113420 1 6.89
CHEMBL2113425 1 6.86
CHEMBL2113426 1 6.80
CHEMBL2113422 1 6.73
CHEMBL2113467 1 6.71
CHEMBL2113437 1 6.68
CHEMBL388757 N6-BENZYLADENOSINE 1 6.26
CHEMBL2113429 1 6.19
CHEMBL477444 1 5.89
CHEMBL2113433 1 5.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL606312 Ki = 7.8 nM 8.11
CHEMBL2113427 Ki = 8.78 nM 8.06
CHEMBL2113428 Ki = 17.5 nM 7.76
CHEMBL66393 Ki = 27.7 nM 7.56
CHEMBL604636 Ki = 31.0 nM 7.51
CHEMBL605468 Ki = 41.0 nM 7.39
CHEMBL2113432 Ki = 44.3 nM 7.35
CHEMBL2113441 Ki = 46.3 nM 7.33
CHEMBL2113468 Ki = 74.0 nM 7.13
CHEMBL263643 Ki = 90.0 nM 7.05
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 120.0 nM 6.92
CHEMBL2113420 Ki = 128.0 nM 6.89
CHEMBL2113425 Ki = 137.0 nM 6.86
CHEMBL2113426 Ki = 159.0 nM 6.80
CHEMBL2113422 Ki = 188.0 nM 6.73
CHEMBL2113467 Ki = 193.0 nM 6.71
CHEMBL2113437 Ki = 211.0 nM 6.68
CHEMBL388757 N6-BENZYLADENOSINE Ki = 550.0 nM 6.26
CHEMBL2113429 Ki = 647.0 nM 6.19
CHEMBL477444 Ki = 1290.0 nM 5.89
CHEMBL2113433 Ki = 1860.0 nM 5.73